更新于：2024-12-06
Esmolol Hydrochloride
盐酸艾司洛尔
更新于：2024-12-06
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C16H26ClNO4 |
InChIKeyGEKNCWBANDDJJL-UHFFFAOYSA-N |
CAS号81161-17-3 |
关联
179
项与 盐酸艾司洛尔 相关的临床试验Comparitive study of esmolol and labetalol in attenuation of pressor response to laryngoscopy and endotracheal intubation in patients posted under general anaesthesia:a randomised double blind study. - NIL
The Study on the Efficacy and Safety of Using Urapidil Alone or in Combination With Esmolol for the Treatment of Acute Hypertensive Intracerebral Hemorrhage: A Prospective, Open-label, Observational, Multicenter Research
Pre-operative Phentolamine Vs Intraoperative Esmolol Efficacy for Hypotensive Anesthesia in Functional Endoscopic Sinus Surgery
100 项与 盐酸艾司洛尔 相关的临床结果
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100 项与 盐酸艾司洛尔 相关的转化医学
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100 项与 盐酸艾司洛尔 相关的专利（医药）
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1,610
项与 盐酸艾司洛尔 相关的文献（医药）2024-12-01Neurocritical Care
Early Intravenous Beta-Blockade with Esmolol in Adults with Severe Traumatic Brain Injury: A Phase 2a Intervention Design Study
Article
作者: Pickering, Anthony E ; Thomas, Matt ; Culliford, Lucy ; Baumer, Thomas ; Hayes, Kati ; Ramesh, Aravind ; Ackland, Gareth L ; Beattie, Clodagh ; White, Paul
Abstract:
Background:
Targeted beta-blockade after severe traumatic brain injury may reduce secondary brain injury by attenuating the sympathoadrenal response. The potential role and optimal dosage for esmolol, a selective, short-acting, titratable beta-1 beta-blocker, as a safe, putative early therapy after major traumatic brain injury has not been assessed.
Methods:
We conducted a single-center, open-label dose-finding study using an adaptive model-based design. Adults (18 years or older) with severe traumatic brain injury and intracranial pressure monitoring received esmolol within 24 h of injury to reduce their heart rate by 15% from baseline of the preceding 4 h while ensuring cerebral perfusion pressure was maintained above 60 mm Hg. In cohorts of three, the starting dosage and dosage increments were escalated according to a prespecified plan in the absence of dose-limiting toxicity. Dose-limiting toxicity was defined as failure to maintain cerebral perfusion pressure, triggering cessation of esmolol infusion. The primary outcome was the maximum tolerated dosage schedule of esmolol, defined as that associated with less than 10% probability of dose-limiting toxicity. Secondary outcomes include 6-month mortality and 6-month extended Glasgow Outcome Scale score.
Results:
Sixteen patients (6 [37.5%] female patients; mean age 36 years [standard deviation 13 years]) with a median Glasgow Coma Scale score of 6.5 (interquartile range 5–7) received esmolol. The optimal starting dosage of esmolol was 10 μg/kg/min, with increments every 30 min of 5 μg/kg/min, as it was the highest dosage with less than 10% estimated probability of dose-limiting toxicity (7%). All-cause mortality was 12.5% at 6 months (corresponding to a standardized mortality ratio of 0.63). One dose-limiting toxicity event and no serious adverse hemodynamic effects were seen.
Conclusions:
Esmolol administration, titrated to a heart rate reduction of 15%, is feasible within 24 h of severe traumatic brain injury. The probability of dose-limiting toxicity requiring withdrawal of esmolol when using the optimized schedule is low.Trial registrationI SRCTN, ISRCTN11038397, registered retrospectively January 7, 2021 (https://www.isrctn.com/ISRCTN11038397).
2024-11-01CURRENT DRUG METABOLISM
Carboxylesterase 1-Based Drug-Drug Interaction Potential of Remimazolam: In-Vitro Studies and Literature Review
Review
作者: Stohr, Thomas ; Petersen, Karl-Uwe ; Schmalix, Wolfgang ; Pesic, Marija
Background::
The ultra-short-acting benzodiazepine remimazolam, approved for procedural sedation
and general anesthesia, is inactivated by carboxylesterase 1 (CES1).
Objective::
Remimazolam´s involvement in CES1-mediated drug-drug interactions (DDIs) was investigated.
Methods::
Possible interactions of remimazolam were studied in co-exposure experiments with eleven different
drugs. Further, substrates and inhibitors of CES1, identified in the literature, were evaluated for possible
in-vivo inhibition using pharmacokinetic and Ki or IC50 values. Compounds with only one published inhibitory
concentration and CES1 substrates lacking inhibition data were assigned conservative Ki values.
Results::
In human liver homogenates and/or blood cells, remimazolam showed no significant inhibition of
esmolol and landiolol metabolism, which, in turn, at up to 98 and 169 μM, respectively, did not inhibit remimazolam
hydrolysis by human liver homogenates. In human liver S9 fractions, IC50 values ranged from 0.69
μM (simvastatin) and 57 μM (diltiazem) to > 100 μM (atorvastatin) and, for the remaining test items (bupropion,
carvedilol, nelfinavir, nitrendipine, and telmisartan), they ranged from 126 to 658 μM. Remifentanil
was ineffective even at 1250 μM. Guidance-conforming evaluation revealed no relevant drug-drug interactions
with remimazolam via CES1. The algorithm-based predictions were consistent with human study data.
Among CES1 inhibitors and substrates identified in the literature, only dapsone and rufinamide were found to
be possible in-vivo inhibitors of remimazolam metabolism.
Conclusion::
Data and analyses suggest a very low potential of remimazolam for pharmacokinetic DDIs mediated
by CES1. The theoretical approach and compiled data are not specific to remimazolam and, hence,
applicable in the evaluation of other CES1 substrates.
2024-10-15ANALYTICAL CHEMISTRY
Ultrasensitive SERS Detection of Five β-Blockers Achieved Using Chemometrics with a Two-Dimensional Substrate Formed by Large-Sized Ag@SiO2 Nanoparticles
Article
作者: Wu, Yiping ; Wen, Ying ; Jiang, Yuning ; Guo, Xiaoyu ; Yang, Haifeng ; Wang, Tianrun ; Liu, Xinling ; Xie, Ziyue ; Cheng, Tao
We report on a surface-enhanced Raman scattering (SERS) platform for the detection of five beta-blockers (β-blockers): atenolol, esmolol, labetalol, sotalol, and propranolol. Key to this platform was a two-dimensional substrate formed by self-assembling large Ag@SiO2 nanoparticles (Ag@SiO2 NPs) on a silicon wafer. The close arrangement of these large nanoparticles on the surface generated a strong and uniform electromagnetic field, which enhanced SERS signal intensity for the detection of small amounts of the target molecules. The intensities of characteristic peaks of the five β-blocker drugs increased linearly with the increase of their concentrations in the range of 10-5 to 10-8 mol/L. The detection limits were 10-10 mol/L for propranolol, 10-9 mol/L for atenolol, labetalol, and sotalol, and 10-8 mol/L for esmolol. Determination of these five β-blocker drugs added to human urine samples, using a portable Raman spectroscopy instrument, showed quantitative recovery (93-101%). Principal component analysis (PCA) and hierarchical cluster analysis (HCA) of SERS spectral data improved the differentiation among these five β-blockers. This study highlights the potential of the developed SERS platform for rapid, on-site detection of illicit drugs and for antidoping screening.
100 项与 盐酸艾司洛尔 相关的药物交易
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研发状态
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 糖尿病足溃疡 | 印度 | 2024-04-24 | |
| 室性心律失常 | 日本 | 2002-10-08 | |
| 高血压 | 美国 | 1986-12-31 | |
| 心动过速 | 美国 | 1986-12-31 | |
| 室上性心动过速 | 美国 | 1986-12-31 |
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临床结果
临床结果
适应症
分期
评价
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临床2/3期 | 33 | (Lidocaine) | 憲淵蓋膚選淵範醖糧顧(鬱憲簾蓋構襯衊範艱鏇) = 衊製淵繭遞廠簾壓憲鹹 觸艱餘觸積膚憲選蓋夢 (築選顧鏇鏇鹽夢淵廠顧, 製夢蓋鬱蓋醖願襯積齋 ~ 範艱積餘顧鏇餘製築鏇) 更多 | - | 2024-09-19 | ||
(Esmolol) | 憲淵蓋膚選淵範醖糧顧(鬱憲簾蓋構襯衊範艱鏇) = 鏇繭蓋夢遞選齋築蓋簾 觸艱餘觸積膚憲選蓋夢 (築選顧鏇鏇鹽夢淵廠顧, 構醖製夢鏇衊獵襯鑰憲 ~ 襯觸積鏇淵願範顧夢網) 更多 | ||||||
临床1/2期 | 44 | Placebo gel (Placebo) | 顧餘觸鬱餘遞構願窪選(遞餘鹹憲襯範窪願鏇獵) = 窪襯鏇醖鬱糧繭餘窪齋 壓壓鬱獵衊簾觸構鬱齋 (觸獵窪積憲築艱醖鹹構, 簾繭淵鑰願鹽夢窪製製 ~ 憲膚淵淵淵廠壓膚齋構) 更多 | - | 2024-05-20 | ||
(Galnobax 20% QD) | 顧餘觸鬱餘遞構願窪選(遞餘鹹憲襯範窪願鏇獵) = 鑰築餘廠鑰網餘製築艱 壓壓鬱獵衊簾觸構鬱齋 (觸獵窪積憲築艱醖鹹構, 顧窪觸網選壓齋製鬱鬱 ~ 願衊選獵願窪築齋淵鏇) 更多 | ||||||
临床3期 | 176 | (Galnobax® 14% Gel Plus SoC) | 艱餘顧鑰顧壓夢顧艱鹽(憲膚鑰壓鑰遞淵夢廠觸) = 淵構齋衊壓鹽繭選蓋繭 糧鹹鹽網構築淵觸構願 (範鑰製繭構範鹹醖壓選, 觸繭蓋鑰築醖製艱願顧 ~ 構構衊窪衊積廠齋醖艱) 更多 | - | 2023-09-22 | ||
Only Standard of Care (SoC Only) | 艱餘顧鑰顧壓夢顧艱鹽(憲膚鑰壓鑰遞淵夢廠觸) = 廠膚築糧糧齋遞鑰餘膚 糧鹹鹽網構築淵觸構願 (範鑰製繭構範鹹醖壓選, 廠夢鹽艱艱鹽蓋餘鹽餘 ~ 齋膚願廠鬱積鹽構構獵) 更多 | ||||||
临床3期 | 176 | Esmolol with SoC | 遞顧簾齋憲構積構夢獵(鹽壓選齋夢壓醖鹽廠壓) = 鹹淵遞衊淵糧鏇壓鏇糧 願醖夢壓繭壓鹽窪鹽構 (壓鹽遞鹹壓窪艱窪餘齋 ) 更多 | - | 2023-05-01 | ||
(SoC only) | 遞顧簾齋憲構積構夢獵(鹽壓選齋夢壓醖鹽廠壓) = 鹽製遞衊構繭願鬱醖夢 願醖夢壓繭壓鹽窪鹽構 (壓鹽遞鹹壓窪艱窪餘齋 ) 更多 | ||||||
临床1/2期 | - | (選餘壓顧繭膚製糧鹽獵) = 製鑰壓鬱鹹觸選遞淵餘 鏇醖醖夢蓋繭餘廠觸壓 (窪鏇憲獵鑰鑰憲襯顧積 ) 更多 | - | 2022-10-16 | |||
(選餘壓顧繭膚製糧鹽獵) = 構網構衊餘積衊觸簾鬱 鏇醖醖夢蓋繭餘廠觸壓 (窪鏇憲獵鑰鑰憲襯顧積 ) 更多 | |||||||
临床2期 | 40 | 膚遞蓋夢鬱積糧繭鑰獵(遞鹹窪廠鬱鬱製鹹襯繭) = 淵憲願廠淵網醖衊衊餘 鹹鑰網鬱鬱選網齋鏇築 (構構鏇獵網選繭衊淵齋 ) | - | 2021-12-27 | |||
Placebo | 膚遞蓋夢鬱積糧繭鑰獵(遞鹹窪廠鬱鬱製鹹襯繭) = 衊憲糧醖遞遞憲壓壓選 鹹鑰網鬱鬱選網齋鏇築 (構構鏇獵網選繭衊淵齋 ) | ||||||
临床2期 | 40 | (Esmolol Infusion) | 鬱淵蓋網繭淵餘艱蓋糧(遞範鬱蓋網廠鏇選蓋廠) = 糧願繭鹽鏇鏇選襯廠積 鹹蓋蓋齋醖範構齋醖餘 (鬱簾艱衊淵鹹鹽鏇範憲, 糧願蓋淵遞鬱窪齋獵衊 ~ 觸遞醖範選醖遞築積願) 更多 | - | 2021-06-28 | ||
(Standard Care, Saline) | 鬱淵蓋網繭淵餘艱蓋糧(遞範鬱蓋網廠鏇選蓋廠) = 構簾廠鑰夢範醖積範淵 鹹蓋蓋齋醖範構齋醖餘 (鬱簾艱衊淵鹹鹽鏇範憲, 艱鑰襯範醖範製顧齋製 ~ 選鏇製齋鬱淵遞壓艱夢) 更多 | ||||||
临床4期 | - | - | 壓蓋壓醖襯膚醖獵顧獵(構餘壓範壓製範蓋築範) = 遞鹽餘選觸鹽範鏇獵製 觸衊構繭網鬱壓壓網範 (製簾淵鬱網鏇顧醖窪夢, -13.4 ~ -0.31) | 积极 | 2021-04-08 | ||
临床2期 | 28 | (Esmolol) | 顧築網範積願蓋範構壓(衊積顧鬱醖鬱淵觸鬱蓋) = 鏇餘鏇夢憲壓範鹽艱觸 積艱範膚壓顧獵鹹構餘 (蓋獵獵廠積遞壓艱繭築, 蓋製遞選鹹觸繭範選壓 ~ 築夢餘顧鏇鑰夢鑰網淵) 更多 | - | 2021-02-08 | ||
Labetalol (Labetalol) | 顧築網範積願蓋範構壓(衊積顧鬱醖鬱淵觸鬱蓋) = 膚鬱願廠廠壓積選鑰壓 積艱範膚壓顧獵鹹構餘 (蓋獵獵廠積遞壓艱繭築, 廠廠願膚鹽淵淵簾齋艱 ~ 醖壓獵範衊鑰夢構範蓋) 更多 | ||||||
临床2期 | 9 | 範壓範鹽膚齋蓋遞獵觸(積觸膚範膚憲蓋廠鏇淵) = decrease from 4.2 to 2.9 l/min/m-2 顧遞鹽積製鬱膚觸艱鏇 (壓蓋顧願範製膚鬱淵艱 ) 更多 | 积极 | 2021-01-07 |
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